Alpha-amylase Inhibitory Activity Research Articles

Proprietary alpha-amylase inhibitor formulation from white kidney bean (Phaseolus vulgaris L.) promotes weight and fat loss: a 12-week, double-blind, placebo-controlled, randomized trial

White kidney bean (Phaseolus vulgaris L.) extracts can aid weight management by reducing calorie intake from complex carbohydrates through alpha-amylase inhibition. We examined the impact of a proprietary aqueous extract from whole dried white kidney beans standardized by its alpha-amylase inhibitor activity (Phase 2 white kidney bean extract (WKBE)) on weight management in subjects with overweight and moderate obesity. In a randomized, double-blind, placebo-controlled fashion, 81 participants completed the study and ingested either a high dose of Phase 2 (1000 mg, WKBE HIGH), a low dose (700 mg, WKBE LOW), or a matching placebo (microcrystalline cellulose, PLA) three times a day, 30 min before meals, for 12 weeks during a calorie restricted diet. In a dose-dependent manner, Phase 2 significantly reduced body weight, fat mass, BMI, waist, hip and in the WKBE HIGH group thigh circumference. Phase 2 is an effective and safe supplement aiding weight and fat loss. ClinicalTrials.gov identifier NCT02930668.

Antioxidant and Alpha Amylase Inhibitory Activity of Apigenin in Alloxan Induced Diabetic Rats

Purpose: to study the antioxidant, inhibitory activity of alpha amylase, antidiabetic, effects of flavonoid Apigeninin in diabetic rats. Methods: The effect of Apigeninon on blood glucose and antioxidant activities were estimated in alloxan induced diabetic and treated rats. The α-amylase inhibitory activity in the serum was assessed after oral administration of 7thday, 14th day, and 21st days treatment of Apigenin. Results: The Apigenin was reduced the serum glucose, α-amylase levels and increased antioxidant levels significantly (P<0.05) in Apigenin alone and combination with Metformin treated groups. Conclusion: The present investigation concludes that flavonoid Apigenin, single drug and combination with Metformin was increased antioxidant and inhibited the alpha-amylase activity and hypoglycemic effect in alloxan induced diabetes rats.

Evaluation of the alpha-amylase inhibitory activity of Euclea natalensis extracts used in the treatment of diabetes mellitus: An experimental and in silico approach

Diabetes, a chronic metabolic disorder with increasing global prevalence, poses a significant public health concern, necessitating the development of safe and effective drugs. This study specifically assessed the inhibitory effects of Euclea natalensis leaf extracts on alpha-amylase through in vitro, in vivo, and in silico methods. The extracts were sequentially obtained using solvents of graded polarity. alpha-amylase inhibition studies were conducted through spectrophotometric methods, while in vivo assessments were performed using a starch tolerance test on rats. Molecular docking was carried out using Autodock 4.2.6, and SwissADME, along with ADMETlab 2.0, were employed to determine the drug-likeness and toxicity properties of the literature-mined compounds. The extracts demonstrated significant in vitro inhibition of alpha-amylase, with the methanol extract exhibiting the highest percentage of inhibition at 27% ± 4.2, followed by hexane and aqueous extracts at 18% ± 2.5 and 18% ± 3.7, respectively. In vivo, the extracts lowered blood glucose levels, with acarbose reducing peak blood glucose levels by 42%, while both the aqueous and methanol extracts reduced it by 19% each after 30 min. The overall glucose-lowering effect, based on the area under the starch tolerance curve, ranked as follows: acarbose > methanol > aqueous > hexane > dichloromethane extract. Molecular docking identified 20(29)-lupene-3 beta-isoferulate C3 as the most promising compound with the lowest binding energy of -11.4 kcal/mol. Molecular dynamics revealed that C3 loses stability as it diverges from the active site. Additionally, while all other compounds passed the Lipinski drug-likeness criteria, 20(29)-lupene-3 beta-isoferulate C3 did not. Therefore, the present study suggests that E. natalensis exhibits antidiabetic properties through the inhibition of alpha-amylase and may serve as a source of potential antidiabetic drug molecules.

Alpha-amylase and Alpha-glucosidase Inhibitory Activities of Philippine Indigenous Medicinal Plants

In the Philippines, medicinal plants still provide the first line of therapeutic remedies and their reported efficacy in traditional treatments provides an opportunity for drug discovery and development. The study aimed to evaluate in vitro commonly used Philippine medicinal plants for their alpha-amylase and alpha-glucosidase inhibitory activities as potential sources of antidiabetic agents. The study emphasised the inhibitory activities of 54 medicinal plants against α-amylase and α-glucosidase enzymes. The findings revealed 7 medicinal plants with the highest alpha-glucosidase inhibitory activity of ≥ 50% and 3 with alpha-amylase inhibitory activity of ≥ 20%. Ethyl acetate extract of Cycas sp. exhibited the highest α-glucosidase inhibitory activity with 83.87% ± 1.52 followed by the aqueous extract of cf. Calyptranthera sp. With 82.07% ± 0.14 with Acarbose as the reference standard (99.71% ± 0.63) at 10µg/mL (w/v) concentration. For the alpha-amylase inhibitory assay, the highest bioactivity was observed in ethyl acetate extract of Curcuma longa L. (39.44% ± 1.56) with Acarbose as the reference standard (51.59% ± 0.98) at 10µg/mL (w/v) concentration. These findings suggest the potential of the above-mentioned plants as sources of alpha-amylase and alpha-glucosidase inhibitors that may be used as antidiabetic agents.

Enhanced Enzyme Inhibitory Effects of the Nanohybrid Eggplant Extract: An Unusual Pharmaceutical Form for Medicinal Plant

Objective: Recently, biosynthesis/synthesis of nanoflowers has become very attractive for chemical and pharmaceutical sciences, and enhanced enzyme activities. Various plant extracts and their active compounds are effectively used as organic component for novel nanoflowers synthesis. Solanum melongena L., commonly known as eggplant in English, a vegetable and medicinal plant belongs to Solanaceae family has several advantages in materials synthesis due to cheap and obtained easily. The aim of this study is to compare the enzyme ((alpha-glucosidase (AGase), alpha-amylase (AAase), tyrosinase (Tyr), acetylcholinesterase (AChE) and butyryl cholinesterase (BChE)) inhibitory effects of the eggplant’ calyx extract and its Solanum-inorganic hybrid nanoflower (Sm-ihNFs) via in vitro experimental methods. 
 Methods: The hybrid nanoflower was formed (NF) with organic molecules, eggplant extract (Sm), and inorganic compounds, copper to enhance the catalytic activities. The inhibition capacities of the eggplant extract, and its hybrid nanoflower were evaluated on selected enzymes (AGase, AAase, Tyr, AChE and BChE) which play significant roles physiologically by in vitro tests in this study. 
 Results: According to inhibition percentages and IC50 values, Sm-ihNFs showed higher inhibitory activities on enzymes other than ache than the plain crude plant extract. Among all the enzymes that were studied, Sm-ihNFs demonstrated significantly higher alpha-glucosidase and alpha-amylase inhibition activities compared to acarbose. And when compared to galanthamine hydrobromide Sm-ihNFs showed higher enzyme inhibition and significant IC50 value. 
 Conclusion: It was thought that Sm-ihNFs prepared from eggplant extract may have promising potential for antidiabetic drug formulations in the future. The hybrid nanoflowers will be promising and guide for the future work in terms of pharmaceutical and cosmeceutical industry.

Fermentation Kinetic and Alpha-Amylase Inhibition Studies of Mao Wine Fermented by Three Commercial Saccharomyces cerevisiae Yeasts

Mao wine is produced from mao (Antidesma thwaitesianum) and is a local beverage promoting Sakon Nakhon province, Thailand. Understanding the fermentation process is necessary in order to enhance the quality of mao wine products. This study aims to examine the kinetics of mao wine fermentation using 3 commercial types of Saccharomyces cerevisiae yeasts, namely Lalvin 71B, Lalvin RC212 and Lalvin K1-V1116, with an initial pH of 3.4, a sweetness of 22 % Brix and a yeast concentration of 0.4 g L–1 in controlled conditions at 25 °C for 10 days. The results revealed that the kinetic models, including logistic, Luedeking-Piret and modified Luedeking-Piret equations, are appropriate for analyzing the kinetics of yeast growth, alcohol production and reducing sugar, respectively. Lalvin K1-V1116 yeast yielded the highest capacity for alcohol production (~113 g L–1), sugar-to-alcohol conversion (45 % conversion), and product efficiency (88 %), indicating its suitability for mao wine production. Furthermore, the investigation of the alpha-amylase inhibitory activity revealed that the IC50 values of mao wine samples were 2.88 - 4.78 mg mL–1, which were roughly 410 - 680 times greater than those of acarbose. These findings revealed the low efficacy of mao wine in inhibiting alpha-amylase activity. Nevertheless, a decrease in the level of inhibition may result in a decreased likelihood of side effects or undesirable reactions. This treatment is especially beneficial for people who have medication sensitivities. Additional research is required in order to substantiate its applicability in the management of type 2 diabetes. HIGHLIGHTS Mao wines were produced by 3 commercial cerevisiae yeast strains Lalvin K1-V1116 yeast exhibits the highest capacity in converting sugar to alcohol Lalvin K1-V1116 is the most suitable yeast for making mao wine The chosen kinetic models are appropriate for kinetic studies of fermentation process The efficacy of Mao wine in inhibiting the activity of alpha-amylase is quite low GRAPHICAL ABSTRACT

Impact of Fermentation on the Phytochemical Content and Biological Properties of Moringa oleifera Lam. Shoot Teas.

This work examined the variation in chemical and biological properties of Moringa oleifera Lam. shoot (MOS) teas prepared under different degrees of fermentation, viz: non-fermented, semi-fermented and fermented. The chemical composition was ascertained via FTIR, GC-MS, total phenolic and total flavonoid content. Also determined were the biological properties, including antioxidant, antimicrobial and alpha-amylase inhibitory activities. The data confirmed that MOS teas were rich in phenolic and flavonoid compounds, with fermented MOS tea displaying the highest phenolic and flavonoid contents. With respect to antioxidant property, all tea extracts exhibited good radical scavenging activities against DPPH⋅, ABTS⋅+ and NO⋅, and the radical scavenging capacity was in the order of non-fermented>semi-fermented>fermented MOS teas. The same trend was also observed for the antimicrobial activities against Staphylococcus aureus and Staphylococcus epidermidis. In contrast, the fermented MOS tea exhibited better α-amylase inhibitory activity compared to the non-fermented and semi-fermented MOS teas.

Biogenic synthesis of silver nanoparticles from the leaf extract of Enicostema axillare (Poir. ex Lam.) A. Raynal and its alpha amylase inhibition activity

Due to its numerous applications, commercial demand for silver nanoparticles produced by biological means is rising. This procedure has no adverse effects, is inexpensive, takes little time, and is non-toxic. The current work uses leaf extracts from Enicostema axillare (Mamajavo) to synthesise silver nanoparticles. The nanoparticles may be characterised by UV–VIS, FT-IR, SEM, TEM, and EDAX. The effectiveness of the screening inhibition assay and alpha-amaylase inhibitory activities is assessed using methanolic leaf extracts and silver nanoparticles. The outcome shows that AgNps exhibit aggregates of grains with a restricted size distribution range between 60 and 80 nm. In comparison to leaf extract, silver nanoparticles made from methanolic leaf extracts have high alpha-amaylase inhibitory action. This study showed that Enicostema axillare's AgNps decrease in the presence of alpha-amylase inhibitors.

Alpha-amylase inhibitory activity of collagen hydrolysate from Asian bullfrog skin and its application in dark chocolate

Alpha-amylase inhibitory activity of collagen hydrolysate from Asian bullfrog skin and its application in dark chocolate

In Vitro Antioxidant and Antidiabetic properties of leaves aqueous extract of Sonchus maritimus

One of the most serious health issues facing worldwide today is diabetes mellitus. Although they have inevitable adverse effects, conventional antidiabetic medications are effective. However, plants might also provide an alternate source of anti-diabetic chemicals. This study was focused on determining the antioxidant activities of the leaves aqueous extract of Sonchus maritimus using 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging activity and ferric reducing ability assay power (FRAP), as well as its antidiabetic activities, which were performed using different protocols, including alpha-amylase inhibitory properties, glucose uptake by yeast cell’s ability, and glucose adsorption capacity. It was noted that S. maritimum extract exhibited moderate activities to scavenge the free radical DPPH and to reduce ferric iron to ferrous iron compared to standard (ascorbic acid). However, the aqueous extract of S. maritimus showed better alpha-amylase inhibitory activity compared to acarbose. It also showed good adsorption strength for binding to glucose molecules. Moreover, the extract showed excellent improvement in glucose uptake by yeast cells at different glucose concentrations in the medium compared to metformin. In conclusion, the aqueous extract of S. maritimus leaves is a promising source of potential antidiabetic compounds that can help prevent diabetes complications and alleviate associated oxidative stress.

Antibacterial and Anti Diabetic Activities of Ethyl Acetate Fractions of Lactobacillus Isolated from Cow and Goat Milk

ABSTRACT: Antibiotics are one of our most important weapons in fighting with bacterial infections and diabetics. Drugs were derived from natural sources that play an important role in the treatment and prevention of human diseases. Traditional fermented foods containing lactic acid bacteria such as milk, yogurt, curd, etc., have historically been consumed by human. Lactobacilli are well known friendly bacteria for their probiotic activities against pathogens. In this investigation cow and goat milk samples were selected and collected for the study. The gram stain was used for morphological identification of Lactobacillus sp. in the two samples. The two isolated Lactobacillus sp. from goat and cow milk samples were subjected to the extraction of secondary metabolites using the solvent ethyl acetate. The two extracts of Lactobacillus spp. those were isolated from cow and goat milk samples, showed antibacterial activity against Escherichia coli, Staphylococcus aureus, Bacillus subtilis and Pseudomonas aeruginosa. The zone of inhibition was assessed by mm. The good results of zones were observed at 1000 and 2000 µg in cow milk and 2000 µg in goat milk extraction. These metabolites were also showed good results in antidiabetic activity using the alpha amylase inhibition activity. The IC50 value has showed moderate activity in the two crude extractions when compared to acarbose standard drug. Therefore, in this investigation the Lactobacillus sp. producing secondary metabolites was good source for the activity of antibacterial and antidiabetic activity.

Coffee silverskin waste as alternative to produce alkaloids with antioxidant, antihemolytic, and alpha-amylase inhibitory activities

Coffee silverskin waste as alternative to produce alkaloids with antioxidant, antihemolytic, and alpha-amylase inhibitory activities

In‐Vitro Investigation of the α‐Amylase Inhibition Activity of Bare Bis‐Benzylidene‐Cyclohexanone Synthesized by a Highly Selective Solvent‐Free Route

AbstractCurrent work reports the highly selective, solvent‐free synthesis of an endorsed bioactive compound, Bis benzylidine cyclohexanone (BBC) through solid acid catalysed cross aldol condensation route and checks its in‐vitro bio activity. The catalytic support (Multiwalled carbon nanotube) employed was synthesized through the highly sophisticated catalytic chemical vapor deposition (CVD) method and simple mechanical grinding strategy was adopted to decorate sulfonic acid on the support. The C1s X‐ray photoelectron peak of at 290.3 eV confirms the effective interaction of sulfonic acid with MWCNT. The sharp and intense desorption peaks observed at approximately 528.7 °C and 655.15 °C in the TPD analysis unmistakably substantiate the strong acidity of the synthesized system. The alpha amylase inhibition activity of the synthesized compound was calculated to be around 88.5 %, which is in par with the commercial drug as it could inhibit only 96 %. Further, the in‐silico (Docking and Molecular Dynamic Simulation) investigations unveiled a new target site for the compound and this can further be studied in detail to advance the applications in drug design. Detailed scrutiny of various parameters was conducted to validate the bioactivity and pharmaceutical potential of the synthesized compound.

Decoding the alpha-amylase inhibitory activity of Garcinia indica Choisy by computational and experimental studies

Garcinia indica Choisy is traditionally used to manage diabetes mellitus, also used in various herbal formulations, and is indicated as an insulin sensitizer. The present study investigates the hydroalcoholic extract of G. indica Choisy rind as an α-amylase inhibitor, followed by the identification of the probable lead hits via a computational approach. LC-MS analyse were carried out. In vitro assays for alpha amylase were performed at concentrations of G. indica ranging from (1000–125 µg/mL) and acarbose (25–1.56 µg/mL) with inhibition times ranging from 5th to 30th min. In silico study was performed based upon the bioactives traced from LC-MS data retrieved from the PubChem database and predicted for probable targets of diabetes mellitus, followed by a drug-likeness score, probable side effects, and an ADMET profile. In addition, molecular docking and the dynamics of the representative complex were explored using AutoDock Vina and Gromac. In vitro study revealed IC50 values of 400.5, 526.07, 728.05, 792.7, 848.3, and 897.5 µg/mL and acarbose displayed IC50 values of <1.56, 6.6, 10.46, 12.6, 14.14, and 15.24 µg/mL respectively. LC-MS analysis identified 17 bioactives, of which 13 showed positive druglikness; among them, 5 bioactives were predicted to modulate AMY2A. The gene set enrichment analysis revealed that AMY2A and gambogic acid possessed high edge counts, with the lowest binding energy of gambogic acid- AMY2A (-11.7 kcal/mol), followed by amentoflavone (-10.6 kcal/mol), volkensiflavone (-9.3 kcal/mol), fukugcide (-8.8 kcal/mol), and garcinol (-7.7 kcal/mol) when compared with acarbose- AMY2A (-7.7 kcal/mol), which also indicates high stability up to 100 ns in molecular simulation. Hydroalcoholic extract of G. indica rind α-amylase inhibitory activity, may be due to the presence of gambogic acid and other bioactives. Thus, it can be speculated that G. indica may possess anti-diabetic activity by reducing the post prandial glucose level. This needs to be further confirmed via enriched fractions or pure substances with inhibitory activity to develop Traditional medicine based new drugs

BIOCHEMICAL EVALUATION OF INDUS VIVA I PULSE NATURAL AYURVEDIC SYRUP AND IT’S IN SILICO – INTERACTION ANALYSIS

Objectives: In developing countries like India, diabetes mellitus and human bone cancer are progressively increasing which is global encumbrance. The objective of the study is to find out the phytoconstituents of Indus Viva I Pulse health drink extract that has undergone classical chemical characterization, molecular docking, anti-diabetic, anticancer, antibacterial and antifungal studies used as traditional and complementary medicine. The study aimed to evaluate the Gas Chromatography–Mass Spectrometry (GC-MS), High-Performance Liquid Chromatography (HPLC), Liquid Chromatography–High Resolution Mass Spectrometry (LC-HRMS), anticancer, antidiabetic and spectral studies that are used to disclose phytochemicals and their medicinal properties. Methods: Infrared (IR), Ultraviolet (UV), 1H-NMR spectroscopic methods, GC-MS, HPLC and LC-HRMS instrumental detections were employed. Molecular docking, anti-diabetic, anticancer, antibacterial and antifungal studies were carried out using AutoDock 4.2.6. software program, α- Amylase method, Mosmann and Disk diffusion method respectively. Results: GC-MS and HPLC chromatogram of methanol extracts exhibited 12 and 6 peaks, respectively, confirming the presence of 12 phytoconstituents in Indus Viva I Pulse health drink (1I–12I). The total phenol and flavonoid content found in the extracted sample of Indus Viva I Pulse health drink were 0.16 and 0.36 mg/mL, respectively. It is a polyherbal formulation of brown-colored liquid of the UV spectrum in methanol is characteristic of an aromatic compound with λ max of 319 and 412 nm. IR spectrum gave peaks at 3,457, 2,922, 2,857, 2,121, 1,641, 1,055, 1,033 and 621 cm-1 indicating the presence of an alcoholic, alkyl, aldehyde or ketone, alkyne, carbonyl, anhydride and methyl group, respectively. Liquid Chromatography- High Resolution Mass Spectrometry (LC-HRMS) study gave these molecular weights (m/z): 1134. 7017, 1150.6475 and 1168.6797. Aromatic characteristics were confirmed through UV, IR, 1H-NMR, 13C-NMR and LC-HRMS spectral studies. 1H-NMR study indicates the presence of aromatic protons and methyl protons. Aqueous extract of Indus Viva I Pulse health drink was tested for Cytotoxicity Assay of human bone cancer (MG-63) cell lines and ptyalin prevent characters that exhibited a valid inhibitory value of 90.87% in 10 μg/mL for MG-63 and value of 74.41% in 500 μg/mL for alpha-amylase which is comparatively more efficient than the available standard drug. Cytotoxicity assay for human bone cancer (MG-63) cell lines and alpha-amylase both showed the inhibitory activity of IC50 68.95 and IC50 36.18 μg/mL, respectively. Conclusion: Based on the result of this research, it can be proposed that Indus Viva I Pulse health drink may serve as a potential remedy for human bone cancer (MG-63) cell line and that alpha-amylase inhibitory activity is proportional to the dose.

Preliminarily investigation on the In-vitro Antimicrobial, Antioxidant and Antidiabetic Activities of Sorindeia warneckei Extracts

Abstract Phytochemicals that are naturally occurring in plants are known to be potentially bioactive, having anti-oxidative, antimicrobial and enzyme inhibiting potentials. This study investigated the antimicrobial, antioxidant and antidiabetic activities of the methanol and dichloromethane extracts of the leaf and stem Sorindeia warneckei. The plant extract showed the presence of saponins, flavonoids, terpenoids, tannins, glycosides, coumarins, steroids, alkaloids, anthraquinones and reducing sugars. The antioxidant potential was evaluated using DPPH radical scavenging assay while the antidiabetic activity was evaluated using an in-vitro α-amylase inhibitory assay. The DPPH free radical scavenging activity was expressed in % inhibition with L Ascorbic acid as standard showing IC50 0.69μg/ml with methanol extract while dichloromethane leaf extract having the highest activity at 0.45μg/ml. The α-amylase assay showed that the extracts exhibited potent alpha amylase inhibitory activity in a dose dependent manner with the leaf methanol extract having an IC50 of 2.33µg/L. The antimicrobial screening using the agar diffusion and agar dilution methods against the bacteria isolates Staphylococcus aureus, Salmonella typhirimurium, Escherichia coli and Streptococcus mutans and the fungal isolates Candida albicans, Aspergillus niger, Aspergillus flavus and Rhizopus oligosporus showed a good positive result. Preliminary investigation reveals that Sorindeia warneckei, contain bioactive compounds that possess promising pharmaceutical potentials that could be exploited.

In vitro study of antioxidant, antigylycation, sugar hydrolysis enzyme inhibitory effect and molecular in silico docking study of angularly condensed diquinothiazines

BackgroundAngularly condensed diquinothiazines (MY1, MY2, and MY3) a phenothiazine derivative was evaluated for antioxidant, antiglycation, sugar hydrolysis enzyme inhibitory effect and molecular in silico docking. MethodAntioxidants were evaluated using DPPH, chelating ion, FRAP and lipid peroxidation. Alpha glucosidase and alpha amylase inhibition was used for sugar hydrolysis enzyme inhibitory activity and antiglycation with BSA-Glucose and BSA-MGO. In silco docking was done with AutoDock Vina and ADMET properties with pkCSM software. ResultAngularly condensed diquinothiazines (MY1, MY2, and MY3) showed free radical scavenging, antiglycation and alpha-glucosidase and alpha-amylase inhibition. Insilco docking and pkCSM ADME shows interaction with aldose reductase, glyoxalase 1, receptor AGE, alpha-glucosidase, and alpha-amylase. ConclusionAntiglycation, alpha-glucosidase, and alpha-amylase inhibition activity of Angularly condensed diquinothiazines maybe through deactivation of aldose reductase enzyme activity, activation of glyoxalase 1 pathway, reduction of dicarbonyl stress and oxidative stress.

Analysis of phytochemical constituent and biological significance of rhododendrons collected from capital of Laliguras, Laliguras municipality, Tehrathum district, Nepal

The largest genus of the Ericaceae family, Rhododendron includes an inspiring number of species. Some of which have been used in the treatment of various ailments such as diseases associated with heart, dysentery, diarrhea, detoxification, fever, constipation, bronchitis and asthma around the world including Nepal. However, systematic study on phytochemistry and pharmacology of Rhododendrons grown in the Capital of Laliguras, Laliguras Municipality, Tehrathum of Nepal is lacking. So this study was conducted to evaluate the antioxidant activity, α-amylase inhibition activity, total phenolic and flavonoid contents of Rhododendron arboretum and Rhododendron campanulatum from Laliguras Municipality, Tehrathum of Nepal. Plant extracts were prepared in methanol by cold percolation method. Phytochemical constituents were analyzed by following standard methods. Antioxidant activity was measured through 2, 2-Diphenyl-1-Picrylhydrazyl assay. Total phenolic and flavonoid content were estimated using Folin–Ciocalteau and aluminum chloride method respectively. Alpha amylase inhibition assay was carried out by starch iodine method. Phytochemical screening of methanolic extract of flower and leaf of R. arboretum and leaves of R. campanulatum displayed the presence of different chemical constituents such as flavonoids, polyphenols, terpenoids, saponins and quinins. Samples showed dose-dependent radical scavenging and α-amylase inhibition activity. Radical scavenging activity and α-amylase inhibition activity of the methanolic extracts of different parts of R. arboretum and R. campanulatum ranged from 19.46 to 95.88% and 13.23 to 68.44% respectively. Flower extracts of R. arboreum showing the strongest radical scavenging activity and α-amylase inhibition with IC50 values 33.61 and 443.44 μg/mL respectively. Among the tested samples, flower extract of R. arboretum showed the strongest antioxidant activity, alpha amylase inhibition activity and contained the highest amount of total phenolic and flavonoid content.&#x0D;

Metabolomics and chemometrics depict the changes in the chemical profile of white lupine (Lupinus albus L.) bioactive metabolites during seed germination.

The current study attempts to illustrate how the chemical and biological profile of white lupine seeds varies throughout the course of various germination days using UHPLC-QqQ-MS combined to chemometrics. Abscisic acid showed maximum level in the un-germinated seeds and started to decline with seed germination accompanied by an increase in the levels of gibberellins which were undetectable in un-germinated seeds. Coumaronochromones were the most prevalent constituents detected in un-germinated seeds while day 2 sprouts showed significant accumulation of flavones. The levels of alkaloids showed significant increase upon germination of the seeds reaching its maximum in day 14 sprouts. The OPLS model coefficients plot indicated that lupinalbin D and F, apigenin hexoside, kaempferol hexoside, albine, and hydoxylupanine showed strong positive correlation to the alpha amylase inhibitory activity of the tested samples while lupinalbin A, lupinisoflavone, lupinic acid and multiflorine were positively correlated to the inhibition of alpha glycosidase activity. The results obtained indicated that seed germination has a profound effect on the chemical profile as well as the in-vitro antidiabetic activity of lupine seeds.

Profiling of Secondary Metabolites from Crassocephalum crepidioides (Wild Leafy Vegetable): Validation of Ethnomedicinal Claim by in-vitro and in-silico Studies

Crassocephalum crepioides, labeled as poor man’s food is one of the neglected and underutilized vegetables in Nigeria. The objective of this paper is therefore to validate the ethnomedicinal claim and profile the secondary metabolites of Crassocephalum crepidioides (Wild Leafy Vegetable) using in-vitro and in-silico investigations. The identification of compounds in the leaf extract with the potential to inhibit 1Z32 alpha-amylase was carried out in-silico. Liquid Chromatography Mass Spectrometry (LCMS) was employed for analysis of the ethanolic leaf extract of this plant, it revealed the presence of sinapic acid, 3-Feruloylquinic acid, dihydroquercetin, malic acid, gallic acid in the extract. Site-directed multi-ligand docking of the identified compounds was performed on 1Z32 protein of alpha-amylase molecular target using the synthetic co-crystallized ligand from the protein. The binding affinity of 3-Feruloylquinic acid (-9.4 kcal/mol) is significantly the highest when compared with sinapic acid (-8.3 kcal/mol). The interactions of this molecule with the amino acids of the protein showed that the mechanism of its inhibitory action is similar to that of the co-crystallized ligand. This study validated an earlier report that the ethanol leaf extract from C. crepidioides showed excellent antidiabetic activity, however, the antidiabetic activity could occur through its alpha-amylase inhibitory activity. Data obtained revealed that C. crepidioides could be an important wild vegetable that could require further advanced exploration rather than neglect.